Phenamil methanesulfonate
Based on 1 Customer Validation
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
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- Pureza : 98.1%
- No. CAS: 1161-94-0
- Fòrmula: C13H16ClN7O4S
- Peso molecular:401.83
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Almacenamiento:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
TRPC3 140 nM (IC50) |
In Vitro
TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca2+-activated channel permeable to Ca2+, Na+, and K+. TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons. Phenamil methanesulfonate (1 μM) decreases 45Ca2+ uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca2+ transport with an IC50 value of 0.28 μM in oocytes expressing TRPP3 or H2O-injected oocytes[1]. Phenamil methanesulfonate is a more potent ENaC blocker than Amiloride, it inhibits the epithelial sodium channel (ENaC) with an IC50 of 400 nM (Amiloride=776 nM)[2].Phenamil methanesulfonate inhibits basal short-circuit currents with IC50 values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells[3].Phenamil methanesulfonate (0-20 μM; 14 days) elevates adipogenic gene expression, PPARγ, Fabp4, and lipoprotein lipase expression in a concentration-dependent manner ,and regulates adipogenesis in C3H10T1/2 cells[4].Phenamil methanesulfonate (0-20 μM; 7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation, it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C3H10T1/2 cells
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Concentration:0 μM and 20 μM
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Incubation Time:14 days
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Result:Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[5]
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Dosage:15 or 30 mg/kg
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Administration:Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
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Result:Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.
Chemical Information
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No. CAS 1161-94-0
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Appearance Solid
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Peso molecular 401.83
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Fòrmula C13H16ClN7O4S
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Color Light yellow to yellow
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SMILES
O=C(C1=NC(Cl)=C(N)N=C1N)NC(NC2=CC=CC=C2)=N.CS(=O)(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (62.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Xiao-Qing Dai , et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. . 2007 Dec;72(6):1576-85. [Content Brief]
[2]. Andrew J Hirsh, et al.Design, synthesis, and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis. J Med Chem. 2006 Jul 13;49(14):4098-115. [Content Brief]
[3]. Andrew J Hirsh, et al.Evaluation of second generation amiloride analogs as therapy for cystic fibrosis lung disease.J Pharmacol Exp Ther. 2004 Dec;311(3):929-38. [Content Brief]
[4]. Mun Chun Chan, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway. Mol Cell Biol [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4886 mL | 12.4431 mL | 24.8861 mL | 62.2154 mL |
| 5 mM | 0.4977 mL | 2.4886 mL | 4.9772 mL | 12.4431 mL | |
| 10 mM | 0.2489 mL | 1.2443 mL | 2.4886 mL | 6.2215 mL | |
| 15 mM | 0.1659 mL | 0.8295 mL | 1.6591 mL | 4.1477 mL | |
| 20 mM | 0.1244 mL | 0.6222 mL | 1.2443 mL | 3.1108 mL | |
| 25 mM | 0.0995 mL | 0.4977 mL | 0.9954 mL | 2.4886 mL | |
| 30 mM | 0.0830 mL | 0.4148 mL | 0.8295 mL | 2.0738 mL | |
| 40 mM | 0.0622 mL | 0.3111 mL | 0.6222 mL | 1.5554 mL | |
| 50 mM | 0.0498 mL | 0.2489 mL | 0.4977 mL | 1.2443 mL | |
| 60 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0369 mL |
Phenamil methanesulfonate Related Classifications
HY-108464A Related Classifications
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